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antibody-drug conjugate CR011-vcMMAE
An antibody-drug conjugate, consisting of the fully human monoclonal antibody CR011 directed against glycoprotein NMB (GPNMB) and conjugated via a cathepsin B-sensitive valine-citrulline (vc) linkage to the cytotoxic agent monomethyl auristatin E (MMAE), with potential antineoplastic activity. Upon administration, CR011 binds to glycoprotein nmb (GPNMB), expressed on the surfaces of a variety of cancer cell types; upon endocytosis, the synthetic dolastin analogue MMAE is released via enzymatic cleavage into the tumor cell cytosol, where it binds to tubulin and inhibits tubulin polymerization, which may result in G2/M phase arrest and apoptosis. The vc linkage system is highly stable in serum, making CR011-vcMMAE ‘s cytotoxicity specific for GPNMB-positive cells. GPNMB is a transmembrane protein overexpressed on the surfaces of various cancer cell types, including melanoma, breast, and prostate cancer cells. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)
| Synonym: | | anti-glycoprotein NMB monoclonal antibody-monomethyl auristatin E conjugate CR011-vcMMAE | | | | Code name: | | CR011-vcMMAE | | |
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